WO2022235699A3 - Potent asgpr-binding compounds for the degradation of immunoglobulins and other proteins - Google Patents

Potent asgpr-binding compounds for the degradation of immunoglobulins and other proteins Download PDF

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Publication number
WO2022235699A3
WO2022235699A3 PCT/US2022/027513 US2022027513W WO2022235699A3 WO 2022235699 A3 WO2022235699 A3 WO 2022235699A3 US 2022027513 W US2022027513 W US 2022027513W WO 2022235699 A3 WO2022235699 A3 WO 2022235699A3
Authority
WO
WIPO (PCT)
Prior art keywords
asgpr
potent
degradation
immunoglobulins
proteins
Prior art date
Application number
PCT/US2022/027513
Other languages
French (fr)
Other versions
WO2022235699A2 (en
Inventor
Jason Allan Wiles
Srinivasa Karra
Mark George Saulnier
Jesse Jingyang CHEN
Kevin Tyler SPROTT
Soumya Ray
Original Assignee
Avilar Therapeutics, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Avilar Therapeutics, Inc. filed Critical Avilar Therapeutics, Inc.
Priority to CN202280047428.4A priority Critical patent/CN117677399A/en
Priority to EP22799448.0A priority patent/EP4334360A2/en
Priority to KR1020237040955A priority patent/KR20240017423A/en
Priority to CA3174145A priority patent/CA3174145A1/en
Priority to AU2022268925A priority patent/AU2022268925A1/en
Publication of WO2022235699A2 publication Critical patent/WO2022235699A2/en
Publication of WO2022235699A3 publication Critical patent/WO2022235699A3/en
Priority to US18/220,737 priority patent/US20240101539A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms

Abstract

Extracellular protein degraders and compositions are provided that have a potent asialoglycoprotein receptor (ASGPR) Binding Ligand bound to an Extracellular Protein Targeting Ligand for the selective degradation of the Target Extracellular Protein, for example immunoglobulin in vivo to treat disorders mediated by the extracellular protein.
PCT/US2022/027513 2021-05-03 2022-05-03 Potent asgpr-binding compounds for the degradation of immunoglobulins and other proteins WO2022235699A2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
CN202280047428.4A CN117677399A (en) 2021-05-03 2022-05-03 Effective ASGPR binding compounds for the degradation of immunoglobulins and other proteins
EP22799448.0A EP4334360A2 (en) 2021-05-03 2022-05-03 Potent asgpr-binding compounds for the degradation of immunoglobulins and other proteins
KR1020237040955A KR20240017423A (en) 2021-05-03 2022-05-03 Potent ASGPR-binding compound for degradation of immunoglobulins and other proteins
CA3174145A CA3174145A1 (en) 2021-05-03 2022-05-03 Potent asgpr-binding compounds for the degradation of immunoglobulins and other proteins
AU2022268925A AU2022268925A1 (en) 2021-05-03 2022-05-03 Potent asgpr-binding compounds for the degradation of immunoglobulins and other proteins
US18/220,737 US20240101539A1 (en) 2021-05-03 2023-07-11 Potent asgpr-binding compounds for the degradation of immunoglobulins and other proteins

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US202163183450P 2021-05-03 2021-05-03
US63/183,450 2021-05-03
US202163228067P 2021-07-31 2021-07-31
US63/228,067 2021-07-31
US202163293447P 2021-12-23 2021-12-23
US63/293,447 2021-12-23
US202263331592P 2022-04-15 2022-04-15
US63/331,592 2022-04-15

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US18/220,737 Continuation US20240101539A1 (en) 2021-05-03 2023-07-11 Potent asgpr-binding compounds for the degradation of immunoglobulins and other proteins

Publications (2)

Publication Number Publication Date
WO2022235699A2 WO2022235699A2 (en) 2022-11-10
WO2022235699A3 true WO2022235699A3 (en) 2022-12-08

Family

ID=83933023

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2022/027513 WO2022235699A2 (en) 2021-05-03 2022-05-03 Potent asgpr-binding compounds for the degradation of immunoglobulins and other proteins

Country Status (6)

Country Link
US (1) US20240101539A1 (en)
EP (1) EP4334360A2 (en)
KR (1) KR20240017423A (en)
AU (1) AU2022268925A1 (en)
TW (1) TW202308703A (en)
WO (1) WO2022235699A2 (en)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4344894A (en) * 1979-07-13 1982-08-17 Imperial Chemical Industries Limited Process for the preparation of cyclopropane carboxylic acid esters
WO2020132100A1 (en) * 2018-12-19 2020-06-25 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules for lysosomal targeting and related compositions and methods
WO2021072269A1 (en) * 2019-10-10 2021-04-15 Yale University Targeted bifunctional degraders
WO2021155317A1 (en) * 2020-01-31 2021-08-05 Avilar Therapeutics, Inc. Asgpr-binding compounds for the degradation of extracellular proteins

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10092549B2 (en) 2013-03-14 2018-10-09 Panoptica, Inc. Ocular formulations for drug-delivery to the posterior segment of the eye
US9884843B2 (en) 2013-12-16 2018-02-06 Peloton Therapeutics, Inc. Cyclic sulfone and sulfoximine analogs and uses thereof

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4344894A (en) * 1979-07-13 1982-08-17 Imperial Chemical Industries Limited Process for the preparation of cyclopropane carboxylic acid esters
WO2020132100A1 (en) * 2018-12-19 2020-06-25 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules for lysosomal targeting and related compositions and methods
WO2021072269A1 (en) * 2019-10-10 2021-04-15 Yale University Targeted bifunctional degraders
WO2021155317A1 (en) * 2020-01-31 2021-08-05 Avilar Therapeutics, Inc. Asgpr-binding compounds for the degradation of extracellular proteins

Also Published As

Publication number Publication date
KR20240017423A (en) 2024-02-07
EP4334360A2 (en) 2024-03-13
WO2022235699A2 (en) 2022-11-10
US20240101539A1 (en) 2024-03-28
TW202308703A (en) 2023-03-01
AU2022268925A1 (en) 2023-11-16

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